Synthesis And Anti-HIV Property of Novel Oligo-DNA Phosphorothioate Analogs Bearing an Intercalative Moiety and/Or Polyamine Residues

Abstract

Novel oligoDNA phosphorothioate analogs (S-ODN-1 to -3) bearing an intercalative moiety at the 5′-terminus and/or polyamine at the C-5 position of certain uridine residues substituting for normal thymidine residues were synthesized and their physicochemical properties as well as the anti-HIV activities were studied. The analogs have identical base sequence which is complementary to art/tris region of human immunodeficiency virus type 1 (HIV-1). The polyamine moiety on the analogs is found to be effective not only to enhance the hybridization ability but also reduce the nonspecific cytotoxicity and strengthen the anti-HIV activity of the analogs.